Wang Pengfei, Zhang Yuman, Zhao Juntong, Yan Yuyue, Liu Liyuan, Zhao Hongwei, He Mingxia
School of Electrical and Information Engineering, Zhengzhou University, Zhengzhou 450001, PR China; Institute of Intelligent Sensing, Zhengzhou University, Zhengzhou 450001, PR China; Henan Key Laboratory of Laser and Opto-electric Information Technology, Zhengzhou University, Zhengzhou 450001, PR China; State Key Laboratory of Precision Measuring Technology and Instruments, Tianjin University, Tianjin 300072, PR China.
School of Electrical and Information Engineering, Zhengzhou University, Zhengzhou 450001, PR China.
Spectrochim Acta A Mol Biomol Spectrosc. 2023 May 5;292:122404. doi: 10.1016/j.saa.2023.122404. Epub 2023 Jan 25.
Cardiovascular pharmaceuticals have drawn huge attention in drug development. Nifedipine (NFD) is an important member of calcium channel blockers (CCB) with the structural characteristic of dihydropyridine (DHP), but the binding mechanism to its target remains an open question. Even though several analytical techniques have been used for structural characterizations, the information of collective vibrational behavior is still lacking. In this work, we use terahertz (THz) spectroscopy to investigate the spectral fingerprints of NFD, and quantitatively evaluate the temperature-induced frequency shifts. Combined with quantum chemical calculations, each THz fingerprint is attributed to specific collective vibrational modes. The collective vibrations of DHP are mainly distributed below 2.5 THz, which provides complementary information to understand the behavior of rigid DHP ring. The rotation of methyl group and the wagging of nitrophenyl group are widely distributed in the range of 1.0-4.0 THz, which is helpful for the conformational recognition between NFD and target molecule. THz spectroscopy is demonstrated to be suitable for characterizing the collective vibrational modes of DHP and elucidating the drug-target binding behavior from the perspective of noncovalent interactions. It has the potential to become a non-invasive technology for conformational analysis and pharmaceutical development.
心血管药物在药物研发中备受关注。硝苯地平(NFD)是钙通道阻滞剂(CCB)的重要成员,具有二氢吡啶(DHP)的结构特征,但其与靶点的结合机制仍是一个未解之谜。尽管已使用多种分析技术进行结构表征,但仍缺乏集体振动行为的信息。在这项工作中,我们使用太赫兹(THz)光谱研究NFD的光谱指纹,并定量评估温度诱导的频率变化。结合量子化学计算,每个THz指纹都归因于特定的集体振动模式。DHP的集体振动主要分布在2.5 THz以下,这为理解刚性DHP环的行为提供了补充信息。甲基的旋转和硝基苯基的摇摆广泛分布在1.0 - 4.0 THz范围内,这有助于NFD与靶分子之间的构象识别。太赫兹光谱被证明适用于表征DHP的集体振动模式,并从非共价相互作用的角度阐明药物 - 靶点结合行为。它有潜力成为一种用于构象分析和药物研发的非侵入性技术。